Nicotine

Registered South African indications:

• Temporary aid to the cigarette smoker seeking to give up the smoking habit

Registered South African contraindications

• Hypersensitivity to the active ingredient or any of its excipients
• Known hypersensitivity of the skin or allergy to nicotine or any of the excipients of nicotine transdermal patch, and generalised skin disorders
• Pregnancy
• Breastfeeding
• In persons during the immediate post-myocardial infarction period (within 3 months)
• In persons with severe, life-threatening cardiac dysrhythmias
• In persons with severe or worsening angina pectoris
• In persons with Prinzmetal’s variant angina
• In persons with stroke in the acute phase
• Women who are planning to fall pregnant

South African recommendations

Caution in the following patient groups

• Severe renal impairment
• Moderate to severe hepatic impairment
• Vasospastic diseases (Buerger’s disease)
• Occlusive peripheral arterial diseases
• Heart failure

Persons diagnosed with the following conditions, should be carefully screened and evaluated, before nicotine transdermal patch is prescribed

Cardiovascular disease

• Serious cardiovascular event, or hospitalisation due to cardiovascular complaint, in the previous 4 weeks (e.g. stroke, myocardial infarction, unstable angina, cardiac dysrhythmia, coronary artery bypass graft and angioplasty) or those who suffer from uncontrolled hypertension
• Patients should be encouraged to stop smoking and non-pharmacological interventions (such as counselling) should be considered
• If this fails, the initiation of pharmacological intervention should be under close medical supervision

Diabetes mellitus

• Patients with diabetes mellitus should be advised to monitor their blood sugar levels more closely than usual when smoking is stopped, and nicotine transdermal patch is initiated as reductions in nicotine-induced catecholamine release can affect carbohydrate metabolism
• Patients with diabetes mellitus may require lower doses of insulin as a result of smoking cessation

Phaeochromocytoma and uncontrolled hyperthyroidism

• Use with caution in patients with uncontrolled hyperthyroidism or phaeochromocytoma as nicotine causes release of catecholamines from the adrenal medulla

Gastrointestinal disease

• Nicotine may exacerbate symptoms in patients suffering from oesophagitis; active duodenal and gastric ulcers
• Nicotine transdermal patch should be used with caution in these conditions

General precautions and warnings

• In case of severe or persistent skin reaction, treatment should be discontinued
• Cigarette smoking is thought to play a perpetuating role in hypertension and peptic ulcer disease, therefore, nicotine transdermal patch should not be used in patients with systemic hypertension or history of peptic ulcer
• Nicotine transdermal patch should not be administered to persons under the age of 18 years of age without recommendation from a health care provider
• Nicotine transdermal patch must be kept out of reach of children at all times i.e. before and after use
• Non-smokers should not use nicotine transdermal patch as they may experience adverse reactions similar to those associated with nicotine administration
• Patients should not smoke whilst using nicotine transdermal patch
• Nicotine transdermal patch should be removed prior to undergoing any magnetic resonance imaging (MRI) procedures to prevent the risk of burns
• If symptoms persist or get worse, or if new symptoms occur, patients should stop use and consult a physician

Transferred dependence

• Transferred dependence can occur but is unusual and is both less harmful and easier to break than smoking dependence

Combination treatment

• Special warnings and precautions for the combination of nicotine transdermal patch with nicotine 2mg chewing gum/ or oromucosal spray 1mg/spray are the same as those for each treatment alone

Effects on ability to drive and use machines

• Nicotine transdermal patch can cause side effects, such as dizziness. Caution is advised before driving a vehicle or operating machinery until the effects of nicotine transdermal patch are known

Forms avail. in SA and covered in this monograph: ptd

South African registered indications and dosages

Temporary aid to the cigarette smoker seeking to give up the smoking habit

• Transdermal (ptd): Following dosage schedule in table below, apply daily to an intact area of the skin upon waking up in the morning and remove at bedtime; Max treatment duration: 6 months

Step	Heavy smokers		Light Smokers
	Dose regimen	Duration	Dose regimen	Duration
Step 1	25mg transdermal patch	First 8 weeks	-	-
Step 2	15mg transdermal patch	Next 2 weeks	15mg transdermal patch	First 8 weeks
Step 3	10mg transdermal patch	Last 2 weeks	10mg transdermal patch	Last 4 weeks

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Nicotine transdermal patch can be used as monotherapy or in combination with 2mg nicotine gum or a 1mg/spray nicotine oromucosal spray

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Patch treatment mimics the fluctuations of nicotine over the day in smokers, with no nicotine administration during sleep. Daytime nicotine patch treatment does not give the nicotine induced sleep disturbances seen with nicotine administration during sleep

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Use of the patch beyond 6 months is generally not recommended

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Smokers should stop smoking completely during the course of treatment with nicotine transdermal patch

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Combination therapy

Highly dependent smokers, smokers who experience breakthrough cravings or those who have failed with single nicotine replacement therapy (NRT), can use nicotine transdermal patch in combination with an oromucosal NRT product for fast relief of cravings. The oromucosal format to consider in combination with the nicotine transdermal patch are 2mg nicotine gum or 1mg/spray nicotine oromucosal spray. Smokers should use the same dosing recommendations for the patch and for the chosen oromucosal format as in monotherapy. For the dosing recommendations for the oromucosal format chosen, refer to Nicotine (CHG) and Nicotine (SPO) 

The dosing schedule for use of the oral pharmaceutical form in combination with the patch is flexible and the users are dosing based on their requirements. For combination therapy, patients are advised to only use one oromucusal format over a 24h period

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See Additional Prescribing Points for method of administration

Not established for use in children

Pregnancy

South African recommendations

• Contraindicated
• Nicotine may cause foetal harm when administered to a pregnant woman, it is therefore contraindicated in women who are or may become pregnant, and female patients should be advised to take adequate precautions to avoid becoming pregnant
• Nicotine passes to the foetus and affects its breathing movements and circulation. The effect on circulation is dose-dependent. Therefore, the pregnant smoker should always be advised to stop smoking completely without use of nicotine replacement therapy
• The risks to the foetus from nicotine transdermal patch are not known. Maternal smoking in pregnancy is associated with low birth weight infants and increased risk of abortion, still birth and neonatal death

Women of childbearing potential/ contraception in males and females

• Contraindicated in women who are planning to fall pregnant (see Contraindications)
• Female patients should be advised to take adequate precautions to avoid becoming pregnant. Consider a pregnancy test before instituting therapy with nicotine transdermal patch

Breastfeeding

South African recommendations

• Contraindicated
• Nicotine passes freely into breast milk in quantities that even at therapeutic doses may affect the infant, therefore the nicotine transdermal patch is contraindicated during lactation or breastfeeding

Fertility

South African recommendations

• In females, tobacco smoking delays time to conception, decreases in vitro fertilisation success rates, and increases risk of infertility
• In males, tobacco smoking reduces sperm production, increases oxidative stress and DNA damage. Spermatozoa from smokers have reduced fertilising capacity. The specific contribution of nicotine however, to these effects in humans, is unknown

South African recommendations

• Mild to moderate: No dose adjustment recommended
• Severe: Caution; no dose adjustment recommended

South African recommendations

• Mild: No dose adjustment recommended
• Moderate to severe: Caution; no dose adjustment recommended

South African recommendations

• No dose adjustment recommended

Immune System Disorders

Less frequent

• Hypersensitivity

Nervous System Disorders

Frequent

• Dizziness
• Headache

Less frequent

• Sleep disorders
• Vivid dreams
• Irritability
• Paraesthesia

Cardiac Disorders

Less frequent

• Palpitations
• Reversible atrial fibrillation

Gastrointestinal Disorders

Frequent

• Gastrointestinal discomfort
• Nausea
• Vomiting
• Constipation

Skin and Subcutaneous Tissue Disorders

Frequent

• Itching
• Erythema

Less frequent

• Urticaria

General Disorders and Administration Site Conditions

Less frequent

• Fatigue

Post-marketing experience

Immune System Disorders

Frequency unknown

• Anaphylactic reaction (systemic effects) 
• Angioedema (systemic effects) 

Psychiatric Disorders

Less frequent

• Abnormal dream (systemic effects, systemic effect, identified only for formulations administered during night) 

Cardiac Disorders

Less frequent

• Tachycardia (systemic effects) 

Vascular Disorders

Less frequent

• Flushing (systemic effects) 
• Hypertension (systemic effects) 

Respiratory, Thoracic and Mediastinal Disorders

Less frequent

• Dyspnoea (systemic effects) 

Skin and Subcutaneous Tissue Disorders

Frequent

• Rash (systemic effects) 
• Urticaria (systemic effects) 

Less frequent

• Hyperhidrosis (systemic effects) 

Musculoskeletal and Connective Tissue Disorders

Less frequent

• Myalgia (in vicinity/region of patch) 

Frequency unknown

• Pain in extremity

General Disorders and Administration Site Conditions

Less frequent

• Application site reaction
• Asthenia (systemic effects) 
• Chest discomfort and pain (systemic effects) 
• Malaise (systemic effects) 

No significant interactions (see Additional Prescribing Points)

None routine. Specific cases may require

• Blood glucose

Method of administration

Nicotine transdermal patch should be applied to clean, dry intact areas of hairless skin, for example on the hip, upper arm, or chest. These areas should be varied each day and the same site should not be used on consecutive days

1. Wash your hands before applying the patch
2. Cut open the pouch with scissors along the side, as indicated. Select a clean, dry, hairless intact area of skin, such as the hip, upper arm or chest
3. Peel one part of the silvery aluminium backing away as far as possible. Avoid touching the sticky surface of the patch with your fingers, as far as possible
4. Apply the sticky part of the patch carefully onto the skin and peel off the remaining half of the silvery aluminium backing
5. Press the patch firmly onto the skin with your palm or finger-tips. Rub your fingers firmly round the edge to ensure that the patch sticks firmly

After removal, used patches should be disposed of carefully. Advice and support improve the success rate

Interaction with other medicines and other forms of interaction

• No clinically relevant interactions between nicotine replacement therapy and other medicines has definitely been established
• However, nicotine may possibly enhance the haemodynamic effects of adenosine, i.e. increase in blood pressure and heart rate and also increase pain response (angina-pectoris type chest pain) provoked by adenosine administration
• Smoking cessation, with or without nicotine substitutes, may alter response to concomitant medicines in ex-smokers
• Smoking (but not nicotine) is considered to increase metabolism and thus lower blood levels of medicines such as caffeine, theophylline, imipramine and pentazocine, through enzyme induction
• Cessation of smoking may result in increased levels of these medicines. Absorption of glutethimide may be decreased and the “first pass” metabolism of propoxyphene decreased by smoking cessation
• Other reported effects of smoking, which do not involve enzyme induction, include reduced diuretic effects of furosemide and decreased cardiac output, and increased blood pressure with propranolol, which may also relate to the hormonal effects of nicotine. Smoking cessation may reverse these actions
• Both smoking and nicotine can increase circulating cortisol and catecholamines. Therapy with adrenergic agonists or with adrenergic blockers may need to be adjusted according to changes in nicotine therapy or smoking status

Nicotine is used in nicotine dependence. Nicotine has both stimulant and depressant phases of action, effected by binding to and acting on a variety of neuro-effector and chemo-sensitive sites, i.e. peripheral nervous system, central nervous system, cardiovascular system, gastrointestinal tract and exocrine glands.

Gum 2mg

• Nicorette (Johnson & Johnson) originator
• Nicorette Mint (Johnson & Johnson) originator

Gum 4mg

• Nicorette (Johnson & Johnson) originator
• Nicorette Mint (Johnson & Johnson) originator

Tablet sublingual 2mg

• Nicorette Microtab (Johnson & Johnson) originator

Patch 5mg

• Nicorette Transdermal Patch  (Johnson & Johnson) originator 

Patch 10mg

• Nicorette Transdermal Patch (Johnson & Johnson) originator 

Patch 15mg

• Nicorette Transdermal Patch  (Johnson & Johnson) originator

Patch 17,5mg/10cm²

• Nicotinell TTS 10 (GSK) originator

Patch 35mg/20cm²

• Nicotinell TTS 20  (GSK) originator

Patch 52.5mg/30cm²

• Nicotinell TTS 30  (Novartis) originator

Spray (per spray) 1:1.0mg, 2:0.66mg, 3:0.33mg, 4:0mg

• Quit 1/2/3/4 (Pharmacare)